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Chemical Compound Review

Redeptin     8-[4,4-bis(4- fluorophenyl)butyl]-1- phenyl...

Synonyms: Fluspirilen, Fluspirilene, Fluspirileno, Imap, Fluspirilenum, ...
 
 
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Disease relevance of Redeptin

  • The difference between the sexes in the potency of fluspirilene and its greater potential to induce parkinsonism may be related to its lesser presynaptic and D1-dopamine receptor blocking properties [1].
  • In recent years concern has been frequently expressed that a long-term treatment with fluspirilene 1.5 mg/week might induce tardive dyskinesia, yet there are no empirical data from controlled studies available [2].
  • Dystonic dysphagia associated with fluspirilene [3].
  • We found no difference between depot fluspirilene and other oral antipsychotics with regard to relapses or to the number of people leaving the study early [4].
  • Though movement disorders (n=60, 1 RCT, RR 31.0 CI 1.9 to 495.6, NNH 4) were found only in the fluspirilene group, there were no convincing data showing the advantage of oral chlorpromazine or other depot antipsychotics over fluspirilene decanoate [4].
 

Psychiatry related information on Redeptin

 

High impact information on Redeptin

 

Chemical compound and disease context of Redeptin

 

Biological context of Redeptin

 

Anatomical context of Redeptin

 

Associations of Redeptin with other chemical compounds

 

Gene context of Redeptin

  • In vitro, all compounds, except the 'typical' antipsychotics haloperidol and fluspirilene, showed higher affinity for 5HT2A than for D2 receptors [15].
  • 1. Recent studies have shown that fluspirilene, a dopamine D2 receptor antagonist which is a long-acting neuroleptic useful in the maintenance therapy of schizophrenic patients, also displays Ca2+ channel blocking activity [10].
  • Conditioned medium also depresses AChE and blocks the development of A12 AChE (Swerts et al., Dev. Biol., 103 (1984) 230-234), but these effects were insensitive to fluspirilene [18].
  • The induction of the vesicular monoamine transporter by high K+ was dependent upon Ca2+ entry through slow calcium channels since it was inhibited by the diphenylbutylpiperidine antagonist fluspirilene and by 20 mM Mg2+, and was enhanced by the dihydropyridine agonist, Bay K8644 [19].
  • Patients with psychosomatic complaints of a hypochondriacal nature were treated with a weekly IM dose of 1.2-1.5 mg fluspirilene (0.6-0.75 ml IMAP) for a period of 10 weeks [20].
 

Analytical, diagnostic and therapeutic context of Redeptin

References

  1. A controlled clinical trial of fluspirilene, a long-acting injectable neuroleptic, in schizophrenic patients with acute exacerbation. Chouinard, G., Annable, L., Steinberg, S. Journal of clinical psychopharmacology. (1986) [Pubmed]
  2. Safety of long-term neuroleptanxiolysis with fluspirilene 1.5 mg per week. Tegeler, J., Lehmann, E., Weiher, A., Heinrich, K. Pharmacopsychiatry (1990) [Pubmed]
  3. Dystonic dysphagia associated with fluspirilene. Stones, M., Kennie, D.C., Fulton, J.D. BMJ (1990) [Pubmed]
  4. Depot fluspirilene for schizophrenia. Abhijnhan, A., Adams, C., David, A., Ozbilen, M. Cochrane database of systematic reviews (Online) (2007) [Pubmed]
  5. Test therapy in the treatment of generalized anxiety disorders with low dose fluspirilene. Wurthmann, C., Klieser, E., Lehmann, E., Pester, U. Prog. Neuropsychopharmacol. Biol. Psychiatry (1995) [Pubmed]
  6. Antischizophrenic drugs of the diphenylbutylpiperidine type act as calcium channel antagonists. Gould, R.J., Murphy, K.M., Reynolds, I.J., Snyder, S.H. Proc. Natl. Acad. Sci. U.S.A. (1983) [Pubmed]
  7. Blockade of low and high threshold Ca2+ channels by diphenylbutylpiperidine antipsychotics linked to inhibition of prolactin gene expression. Enyeart, J.J., Biagi, B.A., Day, R.N., Sheu, S.S., Maurer, R.A. J. Biol. Chem. (1990) [Pubmed]
  8. Substituted diphenylbutylpiperidines bind to a unique high affinity site on the L-type calcium channel. Evidence for a fourth site in the cardiac calcium entry blocker receptor complex. King, V.F., Garcia, M.L., Shevell, J.L., Slaughter, R.S., Kaczorowski, G.J. J. Biol. Chem. (1989) [Pubmed]
  9. Preferential block of T-type calcium channels by neuroleptics in neural crest-derived rat and human C cell lines. Enyeart, J.J., Biagi, B.A., Mlinar, B. Mol. Pharmacol. (1992) [Pubmed]
  10. Inhibition of synaptic transmission and epileptiform activity in central neurones by fluspirilene. Wang, S.J., Lu, K.T., Gean, P.W. Br. J. Pharmacol. (1997) [Pubmed]
  11. A six-month follow-up of refractory chronic psychotics treated with Haldol-AID. Wouters, J. Acta psychiatrica Belgica. (1978) [Pubmed]
  12. Choline high-affinity uptake and metabolism and choline acetyltransferase activity in the striatum of rats chronically treated with neuroleptics. Pedata, F., Sorbi, S., Pepeu, G. J. Neurochem. (1980) [Pubmed]
  13. Selective antagonism of calcium channel activators by fluspirilene. Kenny, B.A., Fraser, S., Kilpatrick, A.T., Spedding, M. Br. J. Pharmacol. (1990) [Pubmed]
  14. Fluspirilene block of N-type calcium current in NGF-differentiated PC12 cells. Grantham, C.J., Main, M.J., Cannell, M.B. Br. J. Pharmacol. (1994) [Pubmed]
  15. Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Schotte, A., Janssen, P.F., Gommeren, W., Luyten, W.H., Van Gompel, P., Lesage, A.S., De Loore, K., Leysen, J.E. Psychopharmacology (Berl.) (1996) [Pubmed]
  16. Abscisic acid plasmalemma perception triggers a calcium influx essential for RAB18 gene expression in Arabidopsis thaliana suspension cells. Ghelis, T., Dellis, O., Jeannette, E., Bardat, F., Miginiac, E., Sotta, B. FEBS Lett. (2000) [Pubmed]
  17. Inhibition of glutamate release by fluspirilene in cerebrocortical nerve terminals (synaptosomes). Wang, S.J. Synapse (2002) [Pubmed]
  18. The role of Ca2+ channels of the L-type in neurotransmitter plasticity of cultured sympathetic neurons. Vidal, S., Raynaud, B., Weber, M.J. Brain Res. Mol. Brain Res. (1989) [Pubmed]
  19. Induction of the vesicular monoamine transporter by elevated potassium concentration in cultures of rat sympathetic neurons. Desnos, C., Raynaud, B., Vidal, S., Weber, M.J., Scherman, D. Brain Res. Dev. Brain Res. (1990) [Pubmed]
  20. Fluspirilene (Imap) in the treatment of psychosomatic complaints in hypochondriacal patients. Kalis, D., Ten Oever, G.H., Erdmann, J.F. Acta psychiatrica Belgica. (1980) [Pubmed]
  21. Unilateral deep brain stimulation of the internal globus pallidus alleviates tardive dyskinesia. Schrader, C., Peschel, T., Petermeyer, M., Dengler, R., Hellwig, D. Mov. Disord. (2004) [Pubmed]
  22. A retrospective evaluation of long-term fluspirilene (IMAP) treatment. Tanghe, A. Acta psychiatrica Belgica. (1976) [Pubmed]
 
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